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Scientific article
English

Asymmetric Synthesis of Pochonin E and F, Revision of Their Proposed Structure, and Their Conversion to Potent Hsp90 Inhibitors

Published inChemistry, vol. 18, no. 29, p. 8978-8986
Publication date2012
Abstract

A concise and modular synthesis of pochonin E and F, and their epimers at C-6 established the correct stereochemistry of these two natural products. Several members of the pochonin family have been shown to bind the heat shock protein 90 (Hsp90), which has been the focus of intense drug discovery efforts. Pochonin E and F as well as their epimers were derivatized into the corresponding pochoximes and further modified at the C-6 position. Molecular dynamics simulations, docking studies, and Hsp90 affinity measurements were performed to evaluate the impact of these modifications.

Keywords
  • conformation analysis
  • Hsp90
  • inhibitors
  • lactones
  • pochonins
Affiliation Not a UNIGE publication
Citation (ISO format)
KARTHIKEYAN, Ganesan et al. Asymmetric Synthesis of Pochonin E and F, Revision of Their Proposed Structure, and Their Conversion to Potent Hsp90 Inhibitors. In: Chemistry, 2012, vol. 18, n° 29, p. 8978–8986. doi: 10.1002/chem.201200546
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Article (Published version)
accessLevelRestricted
Identifiers
ISSN of the journal0947-6539
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Technical informations

Creation12/12/2012 10:41:00 AM
First validation12/12/2012 10:41:00 AM
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